N-butanol Fraction Research Articles

Neuroprotective Effect of Polyphenol Extracts from Terminalia chebula Retz. against Cerebral Ischemia-Reperfusion Injury.

Current therapies for ischemic stroke are insufficient due to the lack of specific drugs. This study aimed to investigate the protective activity of polyphenol extracts from Terminalia chebula against cerebral ischemia-reperfusion induced damage. Polyphenols of ethyl acetate and n-butanol fractions were extracted from T. chebula. BV2 microglial cells exposed to oxygen-glucose deprivation/reoxygenation and mice subjected to middle cerebral artery occlusion/reperfusion were treated by TPE and TPB. Cell viability, cell morphology, apoptosis, mitochondrial membrane potential, enzyme activity and signaling pathway related to oxidative stress were observed. We found that TPE and TPB showed strong antioxidant activity in vitro. The protective effects of TPE and TPB on cerebral ischemia-reperfusion injury were demonstrated by enhanced antioxidant enzyme activities, elevated level of the nucleus transportation of nuclear factor erythroid 2-related factor 2 and expressions of antioxidant proteins, with a simultaneous reduction in cell apoptosis and reactive oxygen species level. In conclusion, TPE and TPB exert neuroprotective effects by stimulating the Nrf2 signaling pathway, thereby inhibiting apoptosis.

Nephroprotective effect of the hydromethanolic extract and fractions of Viola serpens Wall. Histological and hematological evidence

The current study was planned to examine the nephroprotective effect of the crude extract and its various fractions of Viola serpense Wall against paracetamol-induced toxicity in rabbits. The serum creatinine levels of all fractions, as well as the crude extract, were found to have a greater effect. The effect on urine urea by the n-hexane, ethyl acetate, n-butanol and aqueous fraction in high doses (300 mg/kg b.wt.) and crude extract and chloroform in low doses (150 mg/kg bwts.) were comparatively more effective and comparable to silymarin. The creatinine clearance of the fractions except for chloroform, aqueous at 300 mg/kg and the hydro-methanolic extracts at both doses were highly significant. The histological structures of kidneys in crude extract and chloroform-treated groups showed more improvement at the lower doses. The fractions n-hexane, ethyl acetate and n-butanolic exhibited an inverse dose relationship in the histology of the kidney. However, the aqueous fraction showed a dose-dependent nephroprotective effect. Finally, the crude extract and fractions significantly improved paracetamol-induced nephrotoxicity in rabbits.

Investigation into the effect of ethanol leaf extract and fractions of Justicia Secunda on platelets and WBC counts in mice

Aim: This study investigated the effect of the ethanol leaf extract and fractions of Justicia secunda on platelets and WBC counts in mice. Methods: Phytochemical analysis were carried out on the ethanol leaf extract of justicia secunda. A total of 96 apparently healthy mice of different sex were used in this study. Fourteen treated and two control groups of six mice each were used to investigate the effect of leaf extract and fractions of justicia secunda on platelets and white blood cell counts in mice (Groups 1-12) using 20mg/kg/i.p. phenyl-hydrazine (PHZ) daily for 2 days, and then intervention with ethanol extract and 3 fractions (n-hexane, ethylacetate and n-butanol) for 6 days. The positive control group received 20 mg/kg PHZ i.p. only, while the negative control group received food and water only. Blood samples were collected from the retro-orbital plexuses of the mice into EDTA-containing specimen bottles on the 7th day and analyzed for white blood cell (WBC) and platelet (PLT) count. Results: The ethanol leaf extract significantly decreased the platelets and white blood cell count compared to the negative control groups (p< 0.05), they were almost brought back to normal(baseline).The fractions (n-hexane MD, ethyl acetate HD and n-butanol HD) had statistical significant effect on WBC (p< 0.009) in a dose dependent manner. Some of the fractions of J. secunda however had no significant effect on platelets counts (p > 0.146) compared with the control. Conclusion: n-butanol fraction of J. secunda leaf possessed better significant effect on WBC when compared with other fractions, thus, perhaps eliciting immunosuppresant action in the mice.

Antibacterial activity and wound healing potential of Cycas thouarsii R.Br n-butanol fraction in diabetic rats supported with phytochemical profiling

Patients with diabetes mellitus often suffer from chronic wounds due to wound healing impairment. Considering the increased prevalence of diabetes, this would predispose significant medical, economic, and social problems. These chronic wounds are frequently infected with pathogenic bacteria like Pseudomonas aeruginosa, which complicates the situation and makes the wound healing process more difficult. Therefore, there is a high need for therapeutic alternatives to the currently available treatments. Plants are vital sources of many bioactive compounds with multiple biological activities. We elucidated the wound healing possibility and antibacterial effect of Cycas thouarsii n-butanol fraction (CTBF) for the first time. Also, CTBF's phytochemical fingerprint was investigated using the LC-MS/MS technology. Interestingly, CTBF revealed antibacterial activity against P. aeruginosa isolates with minimum inhibitory concentrations range 16–128 µg/mL. Regarding the wound healing potential, we used in vivo experiment on diabetic rats. Remarkably CTBF caused a significant reduction (p 0.05) in the levels of forkhead box O1, matrix metalloproteinases 9, and chemokine (C-C motif) ligand 20. Additionally, it led to a substantial increase (p 0.05) in the level of transforming growth factor β1. Moreover, CTBF improved the wound histological features by increasing the collagen area percentage. Regarding the immunohistochemical studies, CTBF resulted in a strong positive epidermal growth factor and a moderate positive caspase 9 immunoreaction in the epidermis and sebaceous glands of the wounds. Therefore, CTBF could be a promising source of bioactive compounds with wound healing and antibacterial activities. Finally, molecular docking was attempted using MOE software to investigate the binding mode of the major identified compounds in the matrix metalloproteinase 9 (MMP-9) receptor (PDB code: 1GKC).

In vivo investigation of the inhibitory effect of Peganum harmala L. and its major alkaloids on ethylene glycol-induced urolithiasis in rats

Ethnopharmacological relevancePeganum harmala L. is a traditional medicinal plant used for centuries in folk medicine. It has a wide array of therapeutic attributes, which include hypoglycemic, sedative, anti-inflammatory, and antioxidant properties. The fruit decoction of this plant was claimed by Avicenna as traditional therapy for urolithiasis. Also, P. harmala seed showed a clinical reduction in kidney stone number and size in patients with urolithiasis. Aim of the studyIn light of the above-mentioned data, the anti-urolithiatic activities of the seed extracts and the major β-carboline alkaloids of P. harmala were investigated. Materials and methodsExtraction, isolation, and characterization of the major alkaloids were performed using different chromatographic and spectral techniques. The in vivo anti-urolithiatic action was evaluated using ethylene glycol (EG)-induced urolithiasis in rats by studying their mitigating effects on the antioxidant machinery, serum toxicity markers (i.e. nitrogenous waste, such as blood urea nitrogen, uric acid, urea, and creatinine), minerals (such as Ca, Mg, P, and oxalate), kidney injury marker 1 (KIM-1), and urinary markers (i.e. urine pH and urine output). ResultsTwo major alkaloids, harmine (P1) and harmalacidine HCl (P2), were isolated and in vivo evaluated alongside the different extracts. The results showed that P. harmala and its constituents/fractions significantly reduced oxidative stress at 50 mg/kg body weight, p.o., as demonstrated by increased levels of glutathione (GSH), glutathione reductase (GR), glutathione peroxidase (GPx), and catalase (CAT) in kidney homogenate as compared to the EG-treated group. Likewise, the total extract, pet. ether fraction, n-butanol fraction, and P1, P2 alleviated malondialdehyde (MDA) as compared to the EG-treated group. Serum toxicity markers like blood urea nitrogen (BUN), creatinine, uric acid, urea, kidney injury molecule-1 (Kim-1), calcium, magnesium, phosphate, and oxalate levels were decreased by total extract, pet. ether fraction, n-butanol fraction, P1, and P2 as compared to the EG-treated group. Inflammatory markers like NFκ-B and TNF-α were also downregulated in the kidney homogenate of treatment groups as compared to the EG-treated group. Moreover, urine output and urine pH were significantly increased in treatment groups as compared to the EG-treated group deciphering anti-urolithiatic property of P. harmala. Histopathological assessment by different staining patterns also supported the previous findings and indicated that treatment with P. harmala caused a gradual recovery in damaged glomeruli, medulla, interstitial spaces and tubules, and brown calculi materials as compared to the EG-treated group. ConclusionThe current research represents scientific evidence on the use of P. harmala and its major alkaloids as an effective therapy in the prevention and management of urolithiasis.

Characterization of Triadica sebifera (L.) Small Extracts, Antifeedant Activities of Extracts, Fractions, Seed Oil and Isolated Compounds against Plutella xylostella (L.) and Their Effect on Detoxification Enzymes.

Plutella xylostella L. is one of the world’s major pests of cruciferous crops. The indiscriminate use of synthetic insecticides has led to insecticide resistance and resurgence, and has been harmful to non-target organisms and the environment. Botanical insecticides are the best alternatives to synthetic pesticides for the management of pests in organic agriculture and integrated management. T. sebifera is an invasive species and has good potential as an insecticide due to the availability of plant material in some parts of India. The antifeedant activities of T. sebifera have not been reported against P. xylostella and other lepidopteron insects to date. Therefore, the current study targeted the characterization of leaf and bark extracts, feeding deterrence, synergistic and detoxification enzyme activities of leaf/bark ethanolic extracts/fractions, seed oil, and isolated compounds. UHPLC-QTOF-IMS analysis showed that shikimic acid, xanthoxylin, quercetin, kaempferol, methyl gallate, and stigmasterol are common metabolites identified in leaf and bark extracts. The combination of seed oil with bark extract showed higher deterrence (DC50 = 317.10 mg/L) as compared to leaf/bark extracts alone. Gallic acid showed higher deterrence (67.48%) than kaempferol and quercetin. The n-butanol fraction of bark was more repellent (RC50 = 414.61 mg/L). Based on DC50, the seed oil with leaf extract (1:1 ratio) alone with choice and seed oil with leaf and bark extract without choice showed synergistic interaction, but seed oil with bark extract with choice showed additive interaction. The ethanol extract of leaf, bark, and seed oil inhibited GST and AChE in P. xylostella. The leaf extract and seed oil or their combinations may be recommended as antifeedants to reduce damage by P. xylostella based on persistence, antifeedant, phytotoxicity, safety to predators/parasitoids, etc., under field conditions.

Determination of antioxidant activity and tannin content from Aristolochia longa leaves and roots using liquid-liquid fractionation method

Aristolochia longa has been known by its potentiel to cure various diseases.This study was aimd to estimate the antioxidant activity and tannin content of A.longa leaves and roots. Liquid-liquid fractionation by using three solvants was experimented for extraction of tannin from leaves and roots.Then the fractions were oven-dried and powdered to determine the condensed tannin content and antioxidant activity by acidic vanillin, DPPH radical scavenging activity and ferric reducing antioxidant power (FRAP) methods.The qualitative analysis was releazed by high-performance liquid chromatography coupled to mass spectrometry (HPLC DAD-MS).The highest extraction yield was obtained by roots N-butanol fraction (5.15±0.47%).The maximum tannin content value was noted in roots N-butanol fraction (3.90±0.24 mg QUE/g DM) followed by leaves ethyl acetate fraction (3.03±0.01 mg QUE/g DM).The IC50 values of DPPH radical scavenging activity varied significantly from IC50=0.123±0.009mg/ml to 3.737±0.56 mg/ml. Since, the FRAP values ranged from EC50=0.066±0.002 mg/ml to 4,00±0,2 mg/ml. The highest antioxydant ability was observed in leaves and roots N-butanol fractions .Also, the identification by HPLC analysis showed that the roots contains some tannin compounds than leaves such as vescalagin, Roburin D and 1,3,4-tri- O -galloylquinic acid.Our study confirmed the use of A.longa to prevent and control the oxidative stress.

The positive correlation of antioxidant activity and prebiotic effect about oat phenolic compounds

The correlation of antioxidant activity and prebiotic effect about oat phenolic compounds was invested, while there exists limited studies. Free and bound phenolic compounds were separated from ethyl acetate, n-butanol and aqueous fractions. Fluorescence in situ hybridization was used to investigate gut microbiota of in vitro fermentation samples. The results showed that ethyl acetate fraction possesses higher total phenolics contents than that of aqueous fraction (p < 0.01). The bound-n-butanol and free-ethyl acetate fraction exhibited the higher antioxidant capacity (p < 0.01). The phenolic compounds with more powerful antioxidant capacity could promote the proliferation of gut microbiota (Lactobacillus/Enterococcus spp. and Bifidobacterium spp.) (p < 0.05) and inhibit the growth of gut microbiota (Bacteroides spp. and Clostridium/histolyticum group). There is a positive correlation of antioxidant activity and prebiotic effect about oat phenolic compounds. This study provides a basis for the correlation between antioxidant stress and gut microbiota regulation in vivo.

Phytochemical Evaluation and Anti-Inflammatory Potential of Miconia albicans (Sw.) Triana Extracts.

The plant Miconia albicans (Sw.) Triana has been popularly used in Brazil to treat chronic inflammatory disturbances, such as osteoarthritis. This disease affects 250 million people worldwide, and is associated with intense pain and loss of articular function. There is a lack of information about the phytochemistry and bioactivity of M. albicans. Therefore, this study determined the chemical composition of some extracts and evaluated their cytotoxicity, along with their antioxidant and anti-inflammatory, activities using in vitro models. Aqueous and ethanolic extracts were prepared. Afterwards, a liquid–liquid partition was developed using chloroform, ethyl acetate, and n-butanol. The extracts were characterized by LC–MS, and their biological activities were evaluated on epithelial cells (Vero), tumoral hepatic cells (Hep-G2), and THP-1 macrophages. LC–MS analyses identified several flavonoids in all fractions, such as quercetin, myricetin, and their glycosides. The crude extracts and n-butanol fractions did not present cytotoxicity to the cells. The non-toxic fractions presented significant antioxidant activity when evaluated in terms of DPPH scavenging activity, lipid peroxidation, and ROS inhibition. THP-1 macrophages treated with the n-butanol fraction (250 µg/mL) released fewer pro-inflammatory cytokines, even in the presence of LPS. In the future, it will be necessary to identify the phytochemicals that are responsible for anti-inflammatory effects for the discovery of new drugs. In vivo studies on M. albicans extracts are still required to confirm their possible mechanisms of action.

Phytotherapeutic Approach in the Management of Cisplatin Induced Vomiting; Neurochemical Considerations in Pigeon Vomit Model.

Cisplatin induced vomiting involves multiple mechanisms in its genesis and a single antiemetic agent do not cover both the phases (acute & delayed) of vomiting in clinics; necessitating the use of antiemetics in combination. Cannabis sativa and other selected plants have ethnopharmacological significance in relieving emesis. The aim of the present study was to investigate the intrinsic antiemetic profile of Cannabis sativa (CS), Bacopa monniera (BM, family Scrophulariaceae), and Zingiber officinale (ZO, family Zingiberaceae) in combinations against vomiting induced by highly emetogenic anticancer drug-cisplatin in pigeons. We have analysed the neurotransmitters which trigger the vomiting response centrally and peripherally. Electrochemical detector (ECD) was used for the quantification of neurotransmitters and their respective metabolites by high performance liquid chromatography in the brain stem (BS) and area postrema (AP) while peripherally in the small intestine. Cisplatin (7 mg/kg i.v.) induced reliable vomiting throughout the observation period (24 hrs). CS-HexFr (10 mg) + BM-MetFr (10 mg)–Combination 1, BM-ButFr (5 mg) + ZO-ActFr (25 mg)–Combination 2, ZO-ActFr (25 mg) + CS-HexFr (10 mg)–Combination 3, and CS-HexFr (10 mg) + BM-ButFr (5 mg)–Combination 4; provided ~30% (30 ± 1.1), 70% (12 ± 0.4; P < 0.01), 60% (19 ± 0.2; P < 0.05) and 90% (05 ± 0.1; P < 0.001) protection, respectively, against cisplatin induced vomiting as compared to cisplatin control. Standard MCP (30 mg) provided ~50% (23 ± 0.3) protection (P > 0.05). CS Hexane fraction (10 mg/kg), BM methanolic (10 mg/kg) and bacoside rich n-butanol fraction (5 mg/kg) and ZO acetone fraction (25 mg/kg) alone provided ~62%, 36%, 71%, and 44% protection, respectively, as compared to cisplatin control. The most effective and synergistic combination 4 was found to reduce 5HT and 5HIAA (P < 0.05–0.001) in all the brain areas area postrema (AP)+brain stem (BS) and intestine at the 3rd hour of cisplatin administration. In continuation, at the 18th of cisplatin administration reduction in dopamine (P < 0.001) in the AP and 5HT in the brain stem and intestine (P < 0.001) was observed. The said combination did not change the neurotransmitters basal levels and their respective metabolites any significantly. In conclusion, all the tested combinations offered protection against cisplatin induced vomiting to variable degrees, where combination 4 provided enhanced attenuation by antiserotonergic mechanism at the 3rd hour while a blended antidopaminergic and antiserotonergic mechanism at the 18th hour after cisplatin administration.

Multifaced Assessment of Antioxidant Power, Phytochemical Metabolomics, In-Vitro Biological Potential and In-Silico Studies of Neurada procumbens L.: An Important Medicinal Plant.

This work was undertaken to explore the phytochemical composition, antioxidant, and enzyme-inhibiting properties of Neurada procumbens L. extracts/fractions of varying polarity (methanol extract and its fractions including n-hexane, chloroform, n-butanol, and aqueous fractions). A preliminary phytochemical study of all extracts/fractions, HPLC-PDA polyphenolic quantification, and GC-MS analysis of the n-hexane fraction were used to identify the phytochemical makeup. Antioxidant (DPPH), enzyme inhibition (against xanthine oxidase, carbonic anhydrase, and urease enzymes), and antibacterial activities against seven bacterial strains were performed for biological investigation. The GC-MS analysis revealed the tentative identification of 22 distinct phytochemicals in the n-hexane fraction, the majority of which belonged to the phenol, flavonoid, sesquiterpenoid, terpene, fatty acid, sterol, and triterpenoid classes of secondary metabolites. HPLC-PDA analysis quantified syringic acid, 3-OH benzoic acid, t-ferullic acid, naringin, and epicatechin in a significant amount. All of the studied extracts/fractions displayed significant antioxidant capability, with methanol extract exhibiting the highest radical-scavenging activity, as measured by an inhibitory percentage of 81.4 ± 0.7 and an IC50 value of 1.3 ± 0.3. For enzyme inhibition experiments, the n-hexane fraction was shown to be highly potent against xanthine oxidase and urease enzymes, with respective IC50 values of 2.3 ± 0.5 and 1.1 ± 0.4 mg/mL. Similarly, the methanol extract demonstrated the strongest activity against the carbonic anhydrase enzyme, with an IC50 value of 2.2 ± 0.4 mg/mL. Moreover, all the studied extracts/fractions presented moderate antibacterial potential against seven bacterial strains. Molecular docking of the five molecules β-amyrin, campesterol, ergosta-4,6,22-trien-3β-ol, stigmasterol, and caryophyllene revealed the interaction of these ligands with the investigated enzyme (xanthine oxidase). The results of the present study suggested that the N. procumbens plant may be evaluated as a possible source of bioactive compounds with multifunctional therapeutic applications.

A comparative study of nutrient composition, bioactive properties and phytochemical characteristics of Stauntonia obovatifoliola flesh and pericarp.

A comparative study was conducted among the flesh (SOF) and pericarp (SOP) of Stauntonia obovatifoliola, a wild edible fruit in China. The nutrient composition of both these tissues was firstly quantified, and liquid-liquid extraction was then used to separate their methanolic extracts to get petroleum ether, chloroform, ethyl acetate, n-butanol, and residual aqueous fractions, which were evaluated for their total phenol content (TPC), total flavonoid content (TFC), antioxidant capacities, and α-glucosidase and acetylcholinesterase inhibition abilities. Finally, high-performance liquid chromatography (HPLC) was used to analyze their phytochemical composition. The results revealed the excellent nutritional properties of both SOF and SOP, especially SOP (total dietary fiber, 15.50 g/100 g; total amino acids, 0.80 g/100 g; vitamin C, 18.00 mg/100 g; Ca, 272.00 mg/kg; K, 402.00 mg/100 g). For both tissues, their ethyl acetate fractions showed the highest TPC (355.12 and 390.99 mg GAE/g DE) and TFC (306.58 and 298.48 mg RE/g DE). Surprisingly, the ethyl acetate fraction of SOP exhibited the strongest DPPH and ABTS radical scavenging capacity with 1046.94 and 1298.64 mg Trolox/g, respectively, which were higher than that of controls Vc and BHT. In contrast, their chloroform fractions exhibited the strongest ferric reducing antioxidant power (1903.05 and 1407.11 mg FeSO4/g DE) and oxygen radical absorbance capacity (951.12 and 1510.21 mg Trolox/g DE). In addition, the ethyl acetate fraction of SOF displayed superior α-glucosidase inhibition ability with the IC50 value of 0.19 mg/mL, which was comparable to control acarbose. In comparison, the ethyl acetate fraction of SOP had the best acetylcholinesterase inhibition ability with the IC50 value of 0.47 mg/mL. The HPLC analysis results demonstrated that the ethyl acetate fraction of SOP showed significantly higher phenolic content, particularly for phenolic acids (p-hydroxybenzoic acid, 8.00 ± 0.65 mg/g) and flavonoids (epicatechin, 28.63 ± 1.26 mg/g), as compared to other samples. The above results suggest that Stauntonia obovatifoliola, especially its pericarp, had excellent nutrient compositions, bioactive properties and phytochemical characteristics, and had the potential to be developed as natural functional food.

Anti-inflammatory Activity Guided Fractionation of Aerial Parts of Clematis gouriana Roxb. ex DC

Clematis gouriana Roxb. ex DC. also known as Indian Traveler’s Joy is used in different regions of India for curing skin infections, cuts and wounds. The study was performed on 70% methanol extract of C. gouriana aerial parts and its n-hexane, ethyl acetate and n-butanol fractions. The in vitro and in vivo anti-inflammatory potential was evaluated using inhibition of NO production in LPS-stimulated RAW 264.7 macrophages cell line and carrageenan-induced rat paw edema model in vivo, respectively. All the extracts and fractions exhibited concentration-dependent inhibitory effects. It was found that ethyl acetate fraction was the most potent fraction showing 77.24±0.71% inhibition of NO release at 100 μg/mL concentration. The ethyl acetate fraction of C. gouriana also showed significant anti-inflammatory activity in the carrageenan-induced rat paw edema model at a dose of 400 mg/Kg. Further, the phytochemical investigation of the bioactive ethyl acetate fraction led to isolation of five compounds belonging to phenolics and flavonoids type of natural products.

Static Dielectric Constants, Densities, Refractive Indices and Related Properties of Binary Mixtures at Various Temperatures Under Atmospheric Pressure

Experimental dielectric constants at (293.15, 298.15, 303.15) K, densities and refractive indices at 293.15 K are reported for water- ethanol and water- n-butanol binary mixture systems over the entire volume fraction range and atmospheric pressure. From the experimental dielectric data, the excess dielectric constant, effective Kirkwood correlation factor, Bruggeman factor and from density and refractive index data various parameters and their excess properties like excess density, excess refractive index, excess molar polarization, and excess molar volume were estimated and reported in the study. The static dielectric constant of the studied binary mixtures decreases with increase in temperature and volume fraction of the solutes. The density values are decreasing and refractive indices are increasing with increasing volume fraction of ethanol and n-butanol in water. Excess molar volumes values of ethanol and n-butanol are negative over the entire volume fraction range shows the presence of intermolecular interaction and hydrogen bonding in both the binary mixtures.

Bioactivity guided fractionation of &lt;em&gt;Bombax ceib&lt;/em&gt;a L. root extract for antidepressant activity and elucidation of mechanism of action using &lt;em&gt;in silico&lt;/em&gt; studies

The glutamate system has received considerable attention in recent years as a target for development of novel therapeutics, including antidepressants. There are several lines of evidence showing the role of excitatory glutamatergic neurotransmission in depression and antidepressant activity of N-methyl D-aspartate (NMDA) antagonists like ketamine. The excitoxicity induced by glutamate receptor subtype NMDA is selectively and markedly inhibited by hesperidin. The hesperidin is one of the active constituents isolated from the roots of the cotton tree, Bombax ceiba L. (Bombacaceae) . In this context, here, we studied the antidepressant activity of ethanolic extract of root of B. ceiba and its fractions viz., chloroform fraction CBCR (200 &amp; 400 mg/kg); ethyl acetate fraction EABCR (200 &amp; 400 mg/kg); n-butanol fraction (200 &amp; 400 mg/kg) using two animal models of learned helplessness. To further elucidate the possible NMDA antagonist effect of hesperetin, an active metabolite of hesperedin, in silico docking studies were carried out using 5VIH protein of Rattus norvegicus (Brown rat) which consists of GluN1/GluN2A NMDA receptor agonist binding domains, using Inventus v 1.1. Results of in silico study revealed good binding affinity of hesperetin to 5VIH protein. The data indicated antidepressant like activity of the extract and its fractions. The effect was more promising with ethyl acetate and n-butanol fraction of the extract which could be attributed to the antagonistic effect of hesperetin to GluN1/GluN2A NMDA receptor, present in roots of B. ceiba

Exploring potential antidiabetic and anti-inflammatory flavonoids from Euphorbia humifusa with an integrated strategy.

E. humifusa Willd, a monoecious annual plant, native to Eastern Asia, has been traditionally attributed to the treatment and prevention of miscellaneous diseases, including diabetes mellitus and its associated complications. Earlier studies have supported this species’ pharmacological efficacies including its antibacterial, antidiabetic, and anti-inflammatory properties. Even so, the underlying bioactive components with their mechanisms of action associated with its antidiabetic and anti-inflammatory effects remain elusive. The preamble in vitro assessments of the crude extract and its different fractions revealed that the n-butanol fraction (EHNB) exhibited the best activity, which was subsequently subjected to a rapid screening of candidate ligands through bio-affinity ultrafiltration with the two enzyme targets: α-glucosidase (α-Glu) and cycloxygenase-2 (COX-2) combined with UPLC/QTOF-MS. As a result, 7 compounds were identified from EHNB, among them, vitexin and astragalin were screened out as the most active ligand compounds. Vitexin showed great specific binding (SB) affinity values of 1.26 toward α-Glu and 1.32 toward COX-2, while astragalin showed 1.32 and 1.36, respectively. The docking simulation results exhibited strong interactions of vitexin and astragalin with the key residues of the enzyme targets, suggesting their possible mechanisms of action. The in vitro antidiabetic validation revealed noticeable half-maximal inhibitory effects (IC50) of 36.38 ± 3.06 µM for vitexin and 42.47 ± 4.13 µM for astragalin, much better than that of the positive drug acarbose (109.54 ± 14.23 µM). Similarly, these two compounds showed the inhibitory activity against COX-2 with the half-maximal inhibitory effects (IC50) at 27.91 ± 1.74 µM and 49.05 ± 1.49 µM, respectively. Therefore, these two flavonoid compounds (vitexin and astragalin) were speculated as potential antidiabetic and anti-inflammatory compounds from E. humifusa. Taken together, the integrated strategy applied to E. humifusa led to the fast identification of two potential double-acting flavonoids and enlightened its antidiabetic and anti-inflammatory uses. Besides these findings, the integrated strategy in this study could also be used to facilitate the rapid discovery and development of active candidates from other traditional herbal medicines against multi-drug targets and to aid in revealing their mechanisms of action for their traditional uses.

Experimental and numerical study of soot volume fraction and number density in laminar co-flow diffusion flames of n-decane/n-butanol blends

Normal decane was selected as a surrogate fuel for RP-3 aviation fuel, and soot formation characteristics and effects of n-decane (D) /n-butanol (B) cofiring were investigated experimentally and numerically. Combustion experiments of six n-decane/n-butanol blends (i.e., D100, D80, D60, D40, D20, D00, indicating the volumetric fraction of n-butanol in blends) were performed on co-flow diffusion flames. The volume fraction and morphological characteristics of soot at different heights of the flame axis were obtained using thermophoretic sampling and transmission electron microscopy analysis. A newly developed n-decane/n-butanol/PAH kinetic model consisted of 73 species and 275 reactions were further applied to model the soot formation process and ascertain the effects of n-butanol blending. Experimental and simulation results showed that soot loading (soot volume fraction and number density) decreased with increasing n-butanol blending ratios. Chemical kinetic analysis suggested that n-butanol addition decreased the rate of the HACA reaction as a result of a reduction of C2H2 and C2H3 (+M) ⇄ C2H2 + H (+M), ultimately leading to a reduction of soot loading.

ANTIPLASMODIAL ACTIVITIES OF THE STEM BARK EXTRACT OF ARTOCARPUS ALTILIS FORSBERG

Background: The potential of Artocarpus altilis stem bark as a safe antimalarial agent, and the identification of its antimalarial constituents was explored. Materials and Methods:The air-dried stem bark was extracted with 70% ethanol, filtered and concentrated in vacuo to obtain the extract (EE). The extract was successively partitioned to give n-hexane (AAH),dichloromethane (AAD), ethyl acetate (AAE)n-butanol (AAB)and aqueous (AAQ)fractions respectively after determining the acute toxicity using Lorke’s method. These were each evaluated for chemosuppressive antimalarial activities (0-200mg/kg) against chloroquine-sensitive Plasmodium berghei-berghei-infected albino mice. Normal saline and chloroquine, 10 mg/kg were negative and positive control respectively.The survival times and percentage survivors of the mice in both experiments were determined after observation for twenty-eight days post-drug administration. The five (5) column chromatographic (CC) fractions, AAH1, AAH2, AAH3, AAH4andAAH5 obtained from the most active AAH, were also evaluated for antimalarial activities (0-50mg/kg). Further column purification and repeated PTLC of AAH5 yielded three bands, which were finally subjected to GC-MS analysis. Results:EE gave ED50 and LD50 values of 227.17and &gt;5000 mg/kg while its partitioned fractions gave ED50 values as follows: AAH, 79.14; AAD, 215.59;AAE, 160.46,AAB,81.42; and AAQ, 90.85 mg/kg respectively. The primary CC fractions also gave ED50 values as follows:AAH1 21.95;AAH2, 26.96;AAH3,21.30; AAH4, 20.92 andAAH5, 20.75 mg/kg respectively to identify AAH5 as the putative fraction. GC-MS analysis revealed eleven major compounds (1–11) in the three PTLC bands as the antiplasmodial constituents of the plant. Conclusion:The stem bark of A. altilis is a potential agent in malaria control which is safe for oral use.

ANTIPLASMODIAL ACTIVITIES OF THE STEM BARK EXTRACT OF ARTOCARPUS ALTILIS FORSBERG.

Background:The potential of Artocarpus altilis stem bark as a safe antimalarial agent, and the identification of its antimalarial constituents was explored.Materials and Methods:The air-dried stem bark was extracted with 70% ethanol, filtered and concentrated in vacuo to obtain the extract (EE). The extract was successively partitioned to give n-hexane (AAH), dichloromethane (AAD), ethyl acetate (AAE) n-butanol (AAB) and aqueous (AAQ) fractions respectively after determining the acute toxicity using Lorke’s method. These were each evaluated for chemosuppressive antimalarial activities (0-200mg/kg) against chloroquine-sensitive Plasmodium berghei-berghei-infected albino mice. Normal saline and chloroquine, 10 mg/kg were negative and positive control respectively.The survival times and percentage survivors of the mice in both experiments were determined after observation for twenty-eight days post-drug administration. The five (5) column chromatographic (CC) fractions, AAH1, AAH2, AAH3, AAH4 and AAH5 obtained from the most active AAH, were also evaluated for antimalarial activities (0-50mg/kg). Further column purification and repeated PTLC of AAH5 yielded three bands, which were finally subjected to GC-MS analysis.Results:EE gave ED50 and LD50 values of 227.17and >5000 mg/kg while its partitioned fractions gave ED50 values as follows: AAH, 79.14; AAD, 215.59; AAE, 160.46, AAB, .42; and AAQ, 90.85 mg/kg respectively. The primary CC fractions also gave ED50 values as follows: AAH1 21.95; AAH2, 26.96; AAH3, 21.30; AAH4, 20.92 and AAH5, 20.75 mg/kg respectively to identify AAH5 as the putative fraction. GC-MS analysis revealed eleven major compounds (1–11) in the three PTLC bands as the antiplasmodial constituents of the plant.Conclusion:The stem bark of A. altilis is a potential agent in malaria control which is safe for oral use.

Cytotoxic effects of extracts obtained from plants of the Oleaceae family: bio-guided isolation and molecular docking of new secoiridoids from Jasminum humile

Context Traditionally, Oleaceae plants are used to treat many diseases, such as rheumatism, hypercholesterolaemia, or ulcers. Objectives To investigate the cytotoxic potential of Jasminum humile L., Jasminum grandiflorum L., and Olea europaea L. (Oleaceae) extracts against selected human cancer cells lines, followed by a phytochemical investigation of the most potent one. Materials and methods The 95% ethanol extracts of aerial parts of three oleaceous plants were examined for their cytotoxicity against HepG-2, MCF-7, and THP-1 cell lines using MTT assay and doxorubicin (positive control). J. humile was bio-selected and submitted to bio-guided fractionation. Chromatographic workup of ethyl acetate and n-butanol fractions afforded two new compounds; 1-methoxyjasmigenin (1) and 1-methyl-9-aldojasmigenin (2), along with five known ones (3–7). Structures were unambiguously elucidated using 1D/2D NMR and ESI-HRMS. Isolated compounds were assessed for their anti-proliferative potential, and both selectivity index and statistical significance were determined. Molecular docking was conducted against the Mcl-1 receptor using (AZD5991) as a standard. Results Jasmoside (5) was the most potent anticancer compound showing IC50 values of 66.47, 41.32, and 27.59 µg/mL against HepG-2, MCF-7, and THP-1 cell lines, respectively. Moreover, isojasminin (4) exhibited IC50 values of 33.49, 43.12, and 51.07 µg/mL against the same cell lines, respectively. Interestingly, 5 exhibited the highest selectivity index towards MCF-7 and THP-1, even greater than doxorubicin. Molecular docking results were in full agreement with the MTT assay and the proposed SAR. Conclusion In this study, two new compounds were purified. The biological activity highlighted jasmoside (5) as a lead anticancer drug for further future investigation.